Schweinfurthins

Lipid Modulators with Promising Anticancer Activity

Emily J. Koubek, Jillian S. Weissenrieder, Jeffrey Neighbors, Raymond Hohl

Research output: Contribution to journalReview article

1 Citation (Scopus)

Abstract

The schweinfurthin family of compounds displays exciting potent and differential cytotoxicity against human cancer cell lines. Currently, the effect of schweinfurthins on tumor development and progression is being explored in animal models of cancer with promising results. The first schweinfurthin family member, vedelianin, was isolated in 1992, followed by other schweinfurthins in 1998. This opened up the door for the synthesis of additional analogs. At present, the focus of research lies on delineating the mechanism of schweinfurthin action and identifying the nature of sensitivity. It appears that many of the intracellular effects of schweinfurthins are due to, or impacted by, the effect of schweinfurthins on lipid metabolism, synthesis, and homeostasis. These effects include impaired trafficking from the trans-golgi network, disruption of lipid rafts, changes in oxysterol-binding protein activity, and interference with the isoprenoid biosynthesis pathway (IBP). Cancer cells are known to rely heavily on fatty acid, lipid, and sterol synthesis for growth and proliferation. Therefore, compounds that target these needs, such as schweinfurthins, display promise as novel therapeutics. This timely review will take an in-depth look at the history of schweinfurthins, their synthesis, where the research presently stands, and the questions that remain.

Original languageEnglish (US)
Pages (from-to)767-784
Number of pages18
JournalLipids
Volume53
Issue number8
DOIs
StatePublished - Aug 1 2018

Fingerprint

Modulators
Lipids
Neoplasms
Cells
trans-Golgi Network
Biosynthesis
Terpenes
Sterols
Cytotoxicity
Lipid Metabolism
Research
Tumors
Animals
Homeostasis
Fatty Acids
Animal Models
History
Display devices
Cell Line
Growth

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Organic Chemistry
  • Cell Biology

Cite this

Koubek, Emily J. ; Weissenrieder, Jillian S. ; Neighbors, Jeffrey ; Hohl, Raymond. / Schweinfurthins : Lipid Modulators with Promising Anticancer Activity. In: Lipids. 2018 ; Vol. 53, No. 8. pp. 767-784.
@article{4cd50830eb0744f5a05e803bb11721db,
title = "Schweinfurthins: Lipid Modulators with Promising Anticancer Activity",
abstract = "The schweinfurthin family of compounds displays exciting potent and differential cytotoxicity against human cancer cell lines. Currently, the effect of schweinfurthins on tumor development and progression is being explored in animal models of cancer with promising results. The first schweinfurthin family member, vedelianin, was isolated in 1992, followed by other schweinfurthins in 1998. This opened up the door for the synthesis of additional analogs. At present, the focus of research lies on delineating the mechanism of schweinfurthin action and identifying the nature of sensitivity. It appears that many of the intracellular effects of schweinfurthins are due to, or impacted by, the effect of schweinfurthins on lipid metabolism, synthesis, and homeostasis. These effects include impaired trafficking from the trans-golgi network, disruption of lipid rafts, changes in oxysterol-binding protein activity, and interference with the isoprenoid biosynthesis pathway (IBP). Cancer cells are known to rely heavily on fatty acid, lipid, and sterol synthesis for growth and proliferation. Therefore, compounds that target these needs, such as schweinfurthins, display promise as novel therapeutics. This timely review will take an in-depth look at the history of schweinfurthins, their synthesis, where the research presently stands, and the questions that remain.",
author = "Koubek, {Emily J.} and Weissenrieder, {Jillian S.} and Jeffrey Neighbors and Raymond Hohl",
year = "2018",
month = "8",
day = "1",
doi = "10.1002/lipd.12088",
language = "English (US)",
volume = "53",
pages = "767--784",
journal = "Lipids",
issn = "0024-4201",
publisher = "Springer Verlag",
number = "8",

}

Schweinfurthins : Lipid Modulators with Promising Anticancer Activity. / Koubek, Emily J.; Weissenrieder, Jillian S.; Neighbors, Jeffrey; Hohl, Raymond.

In: Lipids, Vol. 53, No. 8, 01.08.2018, p. 767-784.

Research output: Contribution to journalReview article

TY - JOUR

T1 - Schweinfurthins

T2 - Lipid Modulators with Promising Anticancer Activity

AU - Koubek, Emily J.

AU - Weissenrieder, Jillian S.

AU - Neighbors, Jeffrey

AU - Hohl, Raymond

PY - 2018/8/1

Y1 - 2018/8/1

N2 - The schweinfurthin family of compounds displays exciting potent and differential cytotoxicity against human cancer cell lines. Currently, the effect of schweinfurthins on tumor development and progression is being explored in animal models of cancer with promising results. The first schweinfurthin family member, vedelianin, was isolated in 1992, followed by other schweinfurthins in 1998. This opened up the door for the synthesis of additional analogs. At present, the focus of research lies on delineating the mechanism of schweinfurthin action and identifying the nature of sensitivity. It appears that many of the intracellular effects of schweinfurthins are due to, or impacted by, the effect of schweinfurthins on lipid metabolism, synthesis, and homeostasis. These effects include impaired trafficking from the trans-golgi network, disruption of lipid rafts, changes in oxysterol-binding protein activity, and interference with the isoprenoid biosynthesis pathway (IBP). Cancer cells are known to rely heavily on fatty acid, lipid, and sterol synthesis for growth and proliferation. Therefore, compounds that target these needs, such as schweinfurthins, display promise as novel therapeutics. This timely review will take an in-depth look at the history of schweinfurthins, their synthesis, where the research presently stands, and the questions that remain.

AB - The schweinfurthin family of compounds displays exciting potent and differential cytotoxicity against human cancer cell lines. Currently, the effect of schweinfurthins on tumor development and progression is being explored in animal models of cancer with promising results. The first schweinfurthin family member, vedelianin, was isolated in 1992, followed by other schweinfurthins in 1998. This opened up the door for the synthesis of additional analogs. At present, the focus of research lies on delineating the mechanism of schweinfurthin action and identifying the nature of sensitivity. It appears that many of the intracellular effects of schweinfurthins are due to, or impacted by, the effect of schweinfurthins on lipid metabolism, synthesis, and homeostasis. These effects include impaired trafficking from the trans-golgi network, disruption of lipid rafts, changes in oxysterol-binding protein activity, and interference with the isoprenoid biosynthesis pathway (IBP). Cancer cells are known to rely heavily on fatty acid, lipid, and sterol synthesis for growth and proliferation. Therefore, compounds that target these needs, such as schweinfurthins, display promise as novel therapeutics. This timely review will take an in-depth look at the history of schweinfurthins, their synthesis, where the research presently stands, and the questions that remain.

UR - http://www.scopus.com/inward/record.url?scp=85055191939&partnerID=8YFLogxK

UR - http://www.scopus.com/inward/citedby.url?scp=85055191939&partnerID=8YFLogxK

U2 - 10.1002/lipd.12088

DO - 10.1002/lipd.12088

M3 - Review article

VL - 53

SP - 767

EP - 784

JO - Lipids

JF - Lipids

SN - 0024-4201

IS - 8

ER -